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WO2002083064A3 - A method of treating cancer - Google Patents

A method of treating cancer Download PDF

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Publication number
WO2002083064A3
WO2002083064A3 PCT/US2002/010879 US0210879W WO02083064A3 WO 2002083064 A3 WO2002083064 A3 WO 2002083064A3 US 0210879 W US0210879 W US 0210879W WO 02083064 A3 WO02083064 A3 WO 02083064A3
Authority
WO
WIPO (PCT)
Prior art keywords
treating cancer
akt
compound
directed
activity
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2002/010879
Other languages
French (fr)
Other versions
WO2002083064A2 (en
Inventor
Stanley F Barnett
Deborah Defeo-Jones
Kathleen M Haskell
Hans E Huber
Deborah D Nahas
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Priority to AU2002307163A priority Critical patent/AU2002307163B2/en
Priority to US10/473,791 priority patent/US20040106540A1/en
Priority to CA002442264A priority patent/CA2442264A1/en
Priority to JP2002580869A priority patent/JP2004527531A/en
Priority to EP02762009A priority patent/EP1379250A2/en
Publication of WO2002083064A2 publication Critical patent/WO2002083064A2/en
Publication of WO2002083064A3 publication Critical patent/WO2002083064A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Zoology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

The present invention is directed to a method of treating cancer which comprises administration of a compound which selectively inhibits the activity of one or two of the isoforms of Akt, a serine/threonine protein kinase. The invention is particularly directed to the method wherein the compound is dependent on the presence of the plestrin homology domain of Akt for its inhibitory activity.
PCT/US2002/010879 2001-04-10 2002-04-08 A method of treating cancer Ceased WO2002083064A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
AU2002307163A AU2002307163B2 (en) 2001-04-10 2002-04-08 A method of treating cancer
US10/473,791 US20040106540A1 (en) 2001-04-10 2002-04-08 Method of treating cancer
CA002442264A CA2442264A1 (en) 2001-04-10 2002-04-08 A method of treating cancer
JP2002580869A JP2004527531A (en) 2001-04-10 2002-04-08 How to treat cancer
EP02762009A EP1379250A2 (en) 2001-04-10 2002-04-08 A method of treating cancer

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US28278301P 2001-04-10 2001-04-10
US60/282,783 2001-04-10

Publications (2)

Publication Number Publication Date
WO2002083064A2 WO2002083064A2 (en) 2002-10-24
WO2002083064A3 true WO2002083064A3 (en) 2003-02-27

Family

ID=23083095

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/010879 Ceased WO2002083064A2 (en) 2001-04-10 2002-04-08 A method of treating cancer

Country Status (6)

Country Link
US (1) US20040106540A1 (en)
EP (1) EP1379250A2 (en)
JP (1) JP2004527531A (en)
AU (1) AU2002307163B2 (en)
CA (1) CA2442264A1 (en)
WO (1) WO2002083064A2 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7482367B2 (en) 2005-08-30 2009-01-27 Novartis Vaccines And Diagnostics, Inc. Substituted benzimidazoles and methods of their use
US7553854B2 (en) 2006-04-19 2009-06-30 Novartis Vaccines And Diagnostics, Inc. 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
US12480950B2 (en) 2011-07-11 2025-11-25 Regeneron Pharmaceuticals, Inc. AKT-specific capture agents, compositions, and methods of using and making

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002083139A1 (en) * 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2002083140A1 (en) * 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
US20040116433A1 (en) * 2002-04-08 2004-06-17 Owens Andrew Pate Inhibitors of akt activity
JP4394960B2 (en) * 2002-04-08 2010-01-06 メルク エンド カムパニー インコーポレーテッド Akt activity inhibitor
JP2006507299A (en) * 2002-10-30 2006-03-02 メルク　エンド　カムパニー　インコーポレーテッド Inhibitor of Akt activity
CN1768040A (en) 2003-03-28 2006-05-03 伊莱利利公司 Isoquinoline-5-sulfonic acid amides as inhibitors of AKT (protein kinase B)
WO2004086038A2 (en) * 2003-03-28 2004-10-07 Institut Curie A method for screening compounds having the capacity to control tumor cell invasion or metastasis using constitutively active akt
ATE461179T1 (en) * 2003-04-24 2010-04-15 Merck Sharp & Dohme ACT ACTIVITY INHIBITOR
AU2004233828B2 (en) 2003-04-24 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2522430A1 (en) * 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
ATE446752T1 (en) 2003-04-24 2009-11-15 Merck & Co Inc ACT ACTIVITY INHIBITOR
WO2005054202A1 (en) 2003-11-25 2005-06-16 Eli Lilly And Company 7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b)
BRPI0508970A (en) * 2004-03-19 2007-08-21 Penn State Res Found combinatorial methods and compositions for the treatment of melanoma
EP1789557A1 (en) * 2004-07-30 2007-05-30 Altana Pharma AG Method for preparing active kinases containing ph domains
KR20070073791A (en) * 2004-10-18 2007-07-10 암젠 인코포레이티드 Thiadiazole compound and its use method
ES2382814T3 (en) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Cis-4 - [(4-chlorophenyl) sulfonyl] -4- (2,5-difluorophenyl) cyclohexanopropanoic acid for cancer treatment
WO2007087246A2 (en) 2006-01-24 2007-08-02 Merck & Co., Inc. Jak2 tyrosine kinase inhibition
AR064010A1 (en) * 2006-12-06 2009-03-04 Merck & Co Inc AKT ACTIVITY INHIBITORS
EP2132177B1 (en) 2007-03-01 2013-07-17 Novartis AG Pim kinase inhibitors and methods of their use
EA200901548A1 (en) 2007-05-21 2010-06-30 Новартис Аг CSF-1R INHIBITORS, COMPOSITIONS AND APPLICATIONS
CA2693473A1 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
EP2173728A2 (en) 2007-07-17 2010-04-14 Amgen Inc. Heterocyclic modulators of pkb
WO2009032652A1 (en) * 2007-08-31 2009-03-12 Smithkline Beecham Corporation Inhibitors of akt activity
WO2009032653A1 (en) * 2007-08-31 2009-03-12 Smith Kline Beecham Corporation Inhibitors of akt activity
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
WO2011032169A2 (en) * 2009-09-14 2011-03-17 Phusis Therapeutics Inc. Pharmaceutical compositions and formulations including inhibitors of the pleckstrin homology domain and methods for using same
BR112012008849A2 (en) 2009-10-14 2015-09-22 Schering Corp compound, pharmaceutical composition, and use of a compound
PH12012501361A1 (en) 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP3587574B1 (en) 2010-08-17 2022-03-16 Sirna Therapeutics, Inc. Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina)
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
ES2663009T3 (en) 2010-10-29 2018-04-10 Sirna Therapeutics, Inc. Inhibition of RNA-mediated gene expression using short interference nucleic acids (ANic)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
JP2014513949A (en) * 2011-04-20 2014-06-19 トラクソン・リミテッド・ライアビリティ・カンパニー Methods for diagnosing cancer in patients
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
BR112015006990A2 (en) 2012-09-28 2017-07-04 Merck Sharp & Dohme compound, pharmaceutical composition, and use of at least one compound
PL2925888T3 (en) 2012-11-28 2018-03-30 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer
US9340532B2 (en) 2012-12-14 2016-05-17 Phusis Therapeutics, Inc. Methods and compositions for inhibiting CNKSR1
WO2014100065A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
JO3589B1 (en) 2014-08-06 2020-07-05 Novartis Ag Protein kinase c inhibitors and methods of their use
US9913875B2 (en) 2015-03-16 2018-03-13 California Institute Of Technology Botulinum neurotoxin-specific capture agents, compositions, and methods of using and making
WO2016172191A1 (en) 2015-04-20 2016-10-27 Phusis Therapeutics, Inc. Compounds, compositions and methods for inhibiting cnksr1
JOP20190055A1 (en) 2016-09-26 2019-03-24 Merck Sharp & Dohme Anti-cd27 antibodies
EP3519425B1 (en) 2016-09-29 2024-02-28 Indi Molecular, Inc. Compositions for detection, inhibition and imaging of indoleamine 2,3-dioxygenase 1 (ido1) and methods of making and using same
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
AU2018252546B2 (en) 2017-04-13 2025-03-13 Sairopa B.V. Anti-SIRPα antibodies
WO2018232345A1 (en) 2017-06-15 2018-12-20 Indi Molecular, Inc. Il-17f and il-17a-specific capture agents, compositions, and methods of using and making
WO2019094312A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3706742B1 (en) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
MX2021001486A (en) 2018-08-07 2021-07-15 Merck Sharp & Dohme Llc Prmt5 inhibitors.
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
US12201679B2 (en) 2019-04-05 2025-01-21 Institute For Systems Biology Epitope-targeted peptide immunostimulants
WO2020236969A1 (en) 2019-05-20 2020-11-26 Indi Molecular, Inc. Compositions and methods relating to detection, inhibition, and imaging of indoleamine 2,3-dioxygenase 1 (ido1)
AU2020408148B2 (en) 2019-12-17 2025-04-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP4076459A4 (en) 2019-12-17 2023-12-20 Merck Sharp & Dohme LLC PRMT5 INHIBITORS
US12441730B2 (en) 2019-12-17 2025-10-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
US12209142B2 (en) 2020-05-29 2025-01-28 Institute For Systems Biology SARS-CoV-2 epitope-targeted peptide immunostimulants
WO2022098743A1 (en) 2020-11-03 2022-05-12 Indi Molecular, Inc. Compositions, imaging, and therapeutic methods targeting folate receptor 1 (folr1)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7482367B2 (en) 2005-08-30 2009-01-27 Novartis Vaccines And Diagnostics, Inc. Substituted benzimidazoles and methods of their use
US7553854B2 (en) 2006-04-19 2009-06-30 Novartis Vaccines And Diagnostics, Inc. 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
US12480950B2 (en) 2011-07-11 2025-11-25 Regeneron Pharmaceuticals, Inc. AKT-specific capture agents, compositions, and methods of using and making

Also Published As

Publication number Publication date
CA2442264A1 (en) 2002-10-24
EP1379250A2 (en) 2004-01-14
US20040106540A1 (en) 2004-06-03
JP2004527531A (en) 2004-09-09
AU2002307163B2 (en) 2006-06-29
WO2002083064A2 (en) 2002-10-24

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